TABLE 1.
Summary of chemical structure and potency of the tested PDF inhibitors in different assays
| Ro no. | Structure | IC50a (μM)
|
MIC (E. coli DC2)
|
||||
|---|---|---|---|---|---|---|---|
| Fe-PDF (E. coli) | Cell-free TC-TL
|
In vivo TC-TL (BL21) | |||||
| Gel | FlashPlate | μM | μg/ml | ||||
| 06-1467 |  |
0.006 | 0.07 | 0.07 | 1 | 5.2 | 2 |
| 66-0376 | 0.04 | 0.3 | 0.35 | 0.7 | 28 | 4 | |
| 66-6976 | 0.1 | 0.35 | 0.5 | 0.3 | 1.9 | 0.5 | |
| 64-1811 | 20 | >100 | >100 | >500 | >263 | >64 | |
a
IC50 compound concentration required to inhibit 50% of specific activity in the assays. The results for the Fe-PDF enzyme assay and the MIC determination (calculated in micromolar) were taken from Apfel et al. (2). Inhibition of MAP was excluded (IC50 > 10 μM).